• Archives of Pharmacal Research
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• 제28권4호
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• pp.476-482
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• 2005

We investigated the pharmacokinetics of 11-hydroxyaclacinomycin X (ID-6105), a novel anthracycline, after intravenous (i.v.) bolus administration at a multiple dose every 24 h for 5 days in rats. To analyze ID-6105 levels in biological samples, we used an HPLC-based method which was validated in a pharmacokinetic study by suitable criteria. The concentrations of ID-6105 after the multiple administration for 5 days were not significantly different from the results after the single administration. The $t_{1/2\alpha}, t_{l/2\beta}, V_{dss}, and CL_{t}$ after the multiple administration were not significantly different from the values after the single administration. Moreover, the concentrations of ID-6105 1 min at day 1-5 after i.v. bolus multiple administration did not show the significant difference. Of the various tissues, ID-6105 mainly distributed to the kidney, lung, spleen, adrenal gland, and liver after i.v. bolus multiple administration. ID-6105 concentrations in the kidney or lung 2 h after i.v. bolus administration were comparable to the plasma concentration shortly after i.v. bolus administration. However, the ID-6105 concentrations in various tissues 48 h after i.v. bolus administration decreased to low levels. ID-6105 was excreted largely in the bile after i.v. bolus multiple administration at the dose of 3 mg/kg. The amounts of ID-6105 found in the bile by 12 h or in the urine by 48 h after the administration were calculated to be $14.1\% or 4.55\%$ of the initial dose, respectively, indicating that ID-6105 is mostly excreted in the bile. In conclusion, ID-6105 was rapidly cleared from the blood and transferred to tissues, suggesting that ID-6105 might not be accumulated in the blood following i.v. bolus multiple dosages of 3 mg/kg every 24 h for 5 days. By 48 h after i.v. bolus administration, ID-6105 concentrations in various tissues had decreased to very low levels. The majority of ID-6105 appears to be excreted in the bile.

• 동의신경정신과학회지
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• 제4권1호
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• pp.155-164
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• 1993

In this study the author had attempted to establish a correlation among alcohol use and MMPI and lunar cycle. MMPI was carried on 2, April 1992(the last day of the second lunar month) and 15, June 1992(the fifteenth day of the fifth lunar month). These experiments took male and female students who were in WON KWANG University as subjects. The results of it suggested the followings. 1) Drinkers and normal subjects average of T-score in each scales were in a normal scores. 2) In every scales except L,K,Si scales drinkers showed higher scores than normal subjects. There was a significant difference on L, F, Pd, Pa, Sc, Ma scales. 3) On the fifteenth day of the month, drinkers showed Higher T-Scores than normal subjects in every scales excepts L,K,Si scales. There was a significant difference in Ma scale. 4) On the last day of the month, drinkers showed higher T-scores than normal subjects in every scales except L,K,Mf,Si scales. There was a significant difference on L, F, Pd, Sc, Ma scales. 5) Drinkers showed higher than normal subjects in symptom of neurosis and psychosis. As the results of above, human character changes to some extend according to alcohol use. There is a tendency that repeated drinking of college students prone to change into habitual drinking or alcoholic impairment. So controlled drinking among the college students is highly recommended.

• Genomics & Informatics
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• 제19권1호
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• pp.7.1-7.13
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• 2021

Levodopa (L-DOPA) therapy is normally practised to treat motor pattern associated with Parkinson disease (PD). Additionally, several inhibitory drugs such as Entacapone and Opicapone are also cosupplemented to protect peripheral inactivation of exogenous L-DOPA (~80%) that occurs due to metabolic activity of the enzyme catechol-O-methyltransferase (COMT). Although, both Entacapone and Opicapone have U.S. Food and Drug Administration approval but regular use of these drugs is associated with high risk of side effects. Thus, authors have focused on in silico discovery of phytochemicals and evaluation of their effectiveness against human soluble COMT using virtual screening, molecular docking, drug-like property prediction, generation of pharmacophoric property, and molecular dynamics simulation. Overall, study proposed, nine phytochemicals (withaphysalin D, withaphysalin N, withaferin A, withacnistin, withaphysalin C, withaphysalin O, withanolide B, withasomnine, and withaphysalin F) of plant Withania somnifera have strong binding efficiency against human COMT in comparison to both of the drugs i.e., Opicapone and Entacapone, thus may be used as putative bioenhancer in L-DOPA therapy. The present study needs further experimental validation to be used as an adjuvant in PD treatment.

• 분석과학
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• 제13권3호
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• pp.309-314
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• 2000

리튬 용융염($LiC+Li_2O$) 내에 미량으로 존재하는 핵분열생성물을 유도결합 플라스마 원자방출분광기(ICP-AES)를 이용하여 분석하였다. 분석대상 원소 중 감도가 가장 좋은 파장을 선택해 이들 파장에서 리튬 500, 1,000, 2,000 mg/L에 따른 분광학적 간섭 여부를 확인한 결과, 분석원소중 0.1 mg/L 이하의 Y, Nd, Sr, La, Eu의 방출세기는 리튬의 농도가 2,000 mg/L까지 증가시켜도 분광학적 간섭을 받지 않은 반면, Mo, Ba, Ru, Pd, Rh, Zr, Ce는 10% 에서 50% 이상 분광학적 간섭과 매트릭스에 의한 스펙트럼 방해가 나타났다. 리튬 매질로부터 미량 금속원소들을 군분리하기 위하여 모의 용융염 용액을 조제해 암모니아수를 가한 후 분리하고 다시 산처리하여 얻은 용액을 ICP-AES로 회수율을 측정하였다. 분석원소 중 Ru, Y, Rh, Zr, Nd, Ce, La, Eu의 회수율은 90% 이상인 반면 Mo, Ba, Pd, Sr는 낮은 회수율을 보여주었으며, 가해준 암모니아수 양이 증가할수록 회수율이 증가하는 경향을 보였다.

• 폴리머
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• 제34권1호
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• pp.25-31
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• 2010

무전해 니켈 도금법을 사용하여 단분산 폴리스티렌 입자 표면에 니켈이 도금된 고분자 코어/금속 쉘의 복합 입자를 제조하였다. 단분산 입자는 분산중합으로 제조하였는데 사용한 분산매질의 종류에 따라 다양한 크기의 단분산 폴리스티렌 입자를 제조할 수 있었다. 그 중 직경 $3.4\;{\mu}m$ 크기의 단분산 폴리스티렌 입자를 선택하여 무전해 니켈 도금을 시도하였다. 니켈 도금에 영향을 미치는 도금 조건을 파악하기 위하여 활성화제인 $PdCl_2$의 농도, 착화제인 glycine의 농도와 니켈 도금액의 투여 시간에 따른 니켈 도금된 폴리스티렌 복합 입자의 모폴로지를 관찰하였다. 본 연구조건하에서는 $PdCl_2$의 농도 0.4 g/L, glycine 농도 1 M 이상인 경우 폴리스티렌 입자 위에 균일한 두께의 니켈층을 형성하였고 석출되는 니켈도 적었다. 도금 시간 2 시간 중에서 동일양의 도금액을 투여 속도를 달리하며 도금한 경우 모폴로지 상의 뚜렷한 차이는 없었으나 0.15 mL/min 속도로 1시간 동안 투여한 경우가 상대적으로 균일한 도금 특성을 보여 주었다.

• Advances in nano research
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• 제12권6호
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• pp.639-652
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• 2022

The prolyl 3-hydroxylase family member 4 (P3H4), is associated with post-translational modification of fibrillar collagens and aberrantly activated in cancer leading to tumor progression. However, its role in clear cell renal cell carcinoma (ccRCC) is still unknown. Here we reported that P3H4 was highly expressed in renal cancer tissues and significantly positive correlated with poor prognosis. Knockdown of P3H4 inhibited the proliferation, migration and metastasis of renal cancer cells in vitro and in vivo, and also, overexpression of it enhanced the oncogenic process. Mechanistically, P3H4 depletion decreased the levels of GDF15-MMP9 axis and repressed its downstream signaling. Further functional studies revealed that inhibition of GDF15 suppressed renal cancer cell growth and GDF15 recombinant human protein (rhGDF15) supplementation effectively rescued the inhibitory effect induced by P3H4 knockdown. Moreover, decreased levels of MMP9 caused by inhibition of P3H4-GDF15 signaling constrained the expression of PD-L1 and suppression of P3H4 accordingly promoted anti-tumor immunity via stimulating the infiltration of CD4+ and CD8+ T cells in syngeneic mice model. Taken together, our findings firstly demonstrated that P3H4 promotes ccRCC progression by activating GDF15-MMP9-PD-L1 axis and targeting P3H4-GDF15-MMP9 signaling pathway can be a novel strategy of controlling ccRCC malignancy.

• 대한한방내과학회지
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• 제29권2호
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• pp.334-347
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• 2008

Background and Objective : Haeyeol-tang, composed of Houttuyniae Herba, Lonicerae Flos, Taraxaci Herba, and Scrophulariae Radix, is widely used for alleviating the symptom of various kinds of inflammatory pulmonary disease, including asthma and COPD. We want to know whether Haeyeol-tang has an anti-inflammatory effect by analyzing expression of pro-inflammatory cytokines. Materials and Methods : We differentiated the THP-1 cells into macrophage-like cells by treatment with PMA. Inflammation was induced by treatment with LPS and PMA. We found the safe concentration of Haeyeol-tang by using MTS assay and used PD98059 as a negative control for comparison of anti-inflammatory effect of Haeyeol-tang. Results : The RT-PCR analysis results show that the cell survival rate is over 100% within 1 ng/mL to 1 ug/mL of Haeyeol-tang and begins to decrease under 100% at 10 ug/mL. The gene expression of $IL-1{\beta}$, IL-6, IL-8, IL-10, $TNF-{\alpha}$ and $TGF-{\beta}$ levels were down-regulated when Haeyeol-tang was treated at concentrations between 1 ng/mL an 1 ug/mL on monocyte-derived macrophages. Interestingly, 1 ug/mL Haeyeol-tang-treated samples showed that the transcriptional activities of IL-8, $TNF-{\alpha}$, IL-10 and $TGF-{\beta}$ were more down-regulated than those of PD098059 $(TNF-{\alpha}$ inhibitor). At protein level, the ELISA analysis results showed that there were more remarkable (p<0.001) decreases in expression of $IL-1{\beta}$, IL-6, IL-8 and $TNF-{\alpha}$ on both the 1 ug/mL Haeyeol-tang-treated group and the PD98059-treated group than the LPS-treated group. Conclusion : We conclude that Haeyeol-tang has an anti-inflammatory effect by inhibiting expression of pro-inflammatory cytokines and chemokines at mRNA and protein levels. These results may provide us a promising way to care for general inflammatory diseases as well as inflammatory pulmonary disease, including asthma and COPD, with further clinical study.

• 약학회지
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• 제30권6호
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• pp.352-355
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• 1986

Methyl-6-deoxy-$\beta$-L-idopyranoside was prepared in good yield by treatment of methyl 2,3,4-tri-O-benzyl-6-deoxy-$\alpha$-D-xylo-hex-5-enopyranoside with H$_2$ on pd, followed by reaction of Na/NH$_3$ at $-50^{\circ}C$. The ratio of L-idopyranoside and D-glucopyranoside was 7 to 1 in 80.7%. It was confirmed that L-idopyranoside was 1C conformation as being expected.

• Mass Spectrometry Letters
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• 제13권4호
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• pp.146-151
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• 2022

Rotigotine (RTG) is a non-ergot dopamine agonist used to manage the early stage of Parkinson's disease (PD) as transdermal patch. However, the poor medication compliance of PD patients and skin issues related with repeated applications of RTG patches lead to the search for alternative formulations and it also requires appropriate analytical methods for their in vivo evaluation. Thus, here, a sensitive, efficient, and cost-effective method to determine RTG in rat plasma using liquid-liquid extraction (LLE) and multiple reaction monitoring was developed. The use of 20 µL of rat plasma for sample treatment, 8-OH-DPAT as the internal standard, and methyl tert-butyl ether as the LLE solvent in the present method gives it advantages over previous methods for the analysis of RTG in biological samples. The good analytical performance of the developed method was confirmed in specificity, linearity (the coefficient of determination ≥0.999 within 0.1-100 ng/mL), sensitivity (the lower limit of quantitation at 0.1 ng/mL), accuracy (81.00-115.05%), precision (≤10.75%), and recovery (81.00-104.48%) by following the FDA guidelines. Finally, the applicability test of the validated method to the in vivo evaluation of a RTG formulation showed that the present method is the only method which can be accurately applied to that longer than 24 hours, critical for the development of formulations with reduced dosing frequencies. Therefore, the present method could contribute to the development of new RTG formulations helpful to people suffering from PD.

• 한국염색가공학회지
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• 제33권4호
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• pp.250-257
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• 2021

Laundry industry has traditionally been considered an industry that generates large amounts of wastewater and Volatile Organic Compounds(VOCs). This is still the case until now. Household laundry detergents are produced and distributed within the safety regulations on the amount of harmful substances detected. While industrial laundry detergents are often distributed without safety regulations, and even laundry workers manufacture and use them on their own. This contaminates water and air and also threatens the safety of workers. This study is a basic study for distributing eco-friendly detergents(EFD-A) developed through previous studies to the laundry industry. Safety, washability and wastewater quality of EFD-A are evaluated. Three existing commercial detergents(PD1, PD2, LD4) are also evaluated to compare with EFD-A. The safety of detergents is confirmed by the content of optical brightener, VOCs, and arsenic. Washability is evaluated by the difference in reflectance of washed and unwashed artificial soiled fabrics according to detergent concentration, washing temperature, and washing time. TOC is used as the index of assessing the wastewater quality. The results are as follows; EFD-A doesn't contain the optical brighteners, VOCs, and arsenic. The optimal washing conditions for EFD-A are 3 g/L concentration, 40 ℃ washing temperature, and 30 min washing time. The soil removal efficiency is about 71 %, which was similar to or somewhat superior to that of PD1, PD2, and LD4. TOC is 63.5 %, which is about 15 % lower than the discharge limit. Through this study, the developed detergent EFD-A can be used as a safe and eco-friendly detergent for the human body and the environment.